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US 2006/0067997 A1Published application
Phospholipid complexes of lexitropsins, their preparation and use in therapeutic formulations
OwnerFederico Arcamone, Ugo Citernesiinventors
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Abstract
Pharmaceutical formulations constituted by a lexitropsin phospholipidic complex in the form of liposomes, micelles or nanoparticles exhibit optimal pharmacological properties in respect to other formulations containing active principles belonging to the same chemical class in both the topical or parenteral treatment of infectious and/or tumour diseases.
Claims8
A phospholipidic preparation consisting in a release system and a lexitropsin of general formula I
- in which R1 is a functional group, preferably a basic one such as a simple or substituted amidine, a secondary or tertiary amine, a quaternary ammonium group, a simple or substituted guanidine, selected from:
- —C(NH)NH2, —C(NH)NHR3, —NH2, NHR3—N(R3)2, —NR3R4, —NH—C(NH)NH2, —NH—C(NH)NHR3, —N(CH2)4, —N3)3+
- whereas R2 represents an aliphatic, aromatic, or arylaliphatic acylic group, also if substituted with atomic groups containing one or more heteroatoms such as atoms of oxygen, nitrogen, or R2 represents a sequence of one or more residues of 1-methyl-4-aminopyrrole-2-carboxylic acid, acylated or not acylated at the N-terminus, also terminating with a residue of 1-methyl-4-carboxamidopyrrole-2-carboxylic acid or with a residue of analogue aminoacids derived from an heterocycle different from pyrrole selected from furane, imidazole, thiophene, thiazole, or derived from benzene, pyridine, a diazine, pyrimidine, substituted or not at the terminal amino group with an acylic group, or containing, in place of the free or substituted amino group a carboxamido group, and R3 or R4 are equal or different lower alkyl groups C1 to C4,
- the release system being a liposome, a micelle, a nanoparticle, a phospholipidic complex or a supramolecular phospholipidic structure able to incorporate a compound of general structure I in stable and reversible form.
1 more element
Dependencies are inferred from the claim text.